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KYA1797K
- Parent CAS: 851304-36-4
- Soluble in DMSO
- MF: C17H11KN2O6S2
- MW: 442.51
Description
Promotor of β-catenin and Ras degradation (IC50 value 0.75 μM for inhibition of TOPflash activity) that effectively suppresses the growth of CRCs (colorectal cancers) harboring APC and KRAS mutations in vitro and in vivo. KYA1797K binds the RGS domain of axin and enhances the binding affinity of β-catenin or Ras with the β-catenin destruction complex components, leading to simultaneous destabilization of β-catenin and Ras via GSK3β activation. KYA1797 also inhibits ASK1 (IC50 value 0.65 μM for inhibition of apoptosis signal-regulating kinase 1).
More Information
| Parent CAS No. | 851304-36-4 |
|---|---|
| Chemical Name | potassium (Z)-3-(5-((5-(4-nitrophenyl)furan-2-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)propanoate |
| SMILES | S1/C(=CC2=CC=C(C3C=CC([N+]([O-])=O)=CC=3)O2)/C(=O)N(CCC(=O)[O-])C1=S.[K+] |
| MFCD | N.A. |
| InChi | InChI=1S/C17H12N2O6S2.K/c20-15(21)7-8-18-16(22)14(27-17(18)26)9-12-5-6-13(25-12)10-1-3-11(4-2-10)19(23)24;/h1-6,9H,7-8H2,(H,20,21);/q;+1/p-1/b14-9-; |
| InChiKey | PHUNRLYHXGMOLG-WQRRWHLMSA-M |
| CID | 119057297 |
| Short Description | dual ASK1 and Wnt/β-catenin inhibitor |
References
- PH Cha et al. Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. Nat Chem Biol. 2016 Aug;12(8):593-600.
- PH Cha et al. Simultaneous destabilization of β-catenin and Ras via targeting of the axin-RGS domain as a potential therapeutic strategy for colorectal cancer. BMB Rep. 2016 Sep;49(9):455-6.
- GP Volynets et al. Rational design of apoptosis signal-regulating kinase 1 inhibitors: discovering novel structural scaffold. Eur J Med Chem. 2013 Mar;61:104-15.
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